Synthesis and evaluation of 1,4-dihydropyridine derivatives with calcium channel blocking activity

Pflugers Arch. 2014 Jul;466(7):1355-63. doi: 10.1007/s00424-013-1376-z. Epub 2013 Oct 23.

Abstract

1,4-Dihydropyridines (DHPs) are an important class of L-type calcium channel blockers that are used to treat conditions such as hypertension and angina. Their primary target in the cardiovascular system is the Cav1.2 L-type calcium channel isoform, however, a number of DHPs also block low-voltage-activated T-type calcium channels. Here, we describe the synthesis of a series of novel DHP derivatives that have a condensed 1,4-DHP ring system (hexahydroquinoline) and report on their abilities to block both L- and T-type calcium channels. Within this series of compounds, modification of a key ester moiety not only regulates the blocking affinity for both L- and T-type channels, but also allows for the development of DHPs with 30-fold selectivity for T-type channels over the L-type. Our data suggest that a condensed dihydropyridine-based scaffold may serve as a pharmacophore for a new class of T-type selective inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calcium Channel Blockers / chemical synthesis*
  • Calcium Channel Blockers / pharmacology
  • Calcium Channels, L-Type / metabolism
  • Calcium Channels, T-Type / metabolism
  • Dihydropyridines / chemistry
  • Dihydropyridines / pharmacology*
  • HEK293 Cells
  • Humans
  • Rats
  • Structure-Activity Relationship

Substances

  • CACNA1H protein, human
  • Calcium Channel Blockers
  • Calcium Channels, L-Type
  • Calcium Channels, T-Type
  • Dihydropyridines
  • 1,4-dihydropyridine